Synthesis and bioreductive potential of a mono Noxide derivative of the alkylating agent chlorambucil
| Autor: | Schroeder Hl, Chandler Kj, Kirkpatrick Dl |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
Male
Cancer Research Cell Survival High-performance liquid chromatography Cyclic N-Oxides chemistry.chemical_compound Equivalent Tumor Cells Cultured medicine Animals Pharmacology (medical) Rats Wistar Cytotoxicity Pharmacology Chlorambucil Chemistry Neoplasms Experimental Hydrogen-Ion Concentration Hypoxia (medical) Cell Hypoxia In vitro Rats Oncology Biochemistry Microsomes Liver Microsome medicine.symptom Oxidation-Reduction Derivative (chemistry) medicine.drug |
| Zdroj: | Anti-Cancer Drugs. 5:467-472 |
| ISSN: | 0959-4973 |
| DOI: | 10.1097/00001813-199408000-00013 |
| Popis: | Chlorambucil N-oxide (CHLN-O) was synthesized and evaluated for in vitro bioreductive antitumor activity. A time-dependent hypoxic differential was observed when EMT6 cells were exposed to CHLN-O in the presence of rat liver microsomes and reducing equivalents. The cytotoxicity of the N-oxide was potentiated under hypoxia, and augmented further by a combination of low pH and hypoxia. Metabolic studies were also undertaken, which utilized previously described HPLC methodology for the analysis of CHLN-O loss from biological fluids. These demonstrated the requirement for microsomal enzymes and reducing equivalents, and also illustrated the time-dependent manner of CHLN-O loss from isolated microsomal preparations. |
| Databáze: | OpenAIRE |
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